Antiretroviral and cytotoxic activities of Tityus obscurus synthetic peptide

Arch Pharm (Weinheim). 2020 Nov;353(11):e2000151. doi: 10.1002/ardp.202000151. Epub 2020 Jul 19.

Abstract

New drugs are constantly in demand, and nature's biodiversity is a rich source of new compounds for therapeutic applications. Synthetic peptides based on the transcriptome analysis of scorpion venoms of Tityus obscurus, Opisthacanthus cayaporum, and Hadrurus gertschi were assayed for their cytotoxic and antiretroviral activity. The Tityus obscurus scorpion-derived synthetic peptide (FFGTLFKLGSKLIPGVMKLFSKKKER), in concentrations ranging from 6.24 to 0.39 μM, proved to be the most active one against simian immunodeficiency virus (SIV) replication in the HUT-78 cell line and in primary human leukocytes, with the lowest toxicity for these cells. The immune cellular response evaluated in primary human leukocytes treated with the most promising peptide and challenged with SIV infection exhibited production of cytokines such as interleukin (IL)-4, IL-6, IL-8, IL-10, and interferon-γ, which could be involved in cell defense mechanisms to overcome viral infection through proinflammatory and anti-inflammatory pathways, similar to those evoked for triggering the mechanisms exerted by antiviral restriction factors.

Keywords: SIV; Tityus obscurus; antiretroviral activity; cytokines; cytotoxicity; retrovirus; synthetic peptides.

MeSH terms

  • Animals
  • Anti-Retroviral Agents / chemical synthesis
  • Anti-Retroviral Agents / pharmacology*
  • Anti-Retroviral Agents / toxicity
  • Cell Line
  • Cell Survival / drug effects
  • Cytokines / metabolism
  • Host-Pathogen Interactions
  • Humans
  • Inflammation Mediators / metabolism
  • Leukocytes / drug effects*
  • Leukocytes / immunology
  • Leukocytes / metabolism
  • Leukocytes / virology
  • Peptides / chemical synthesis
  • Peptides / pharmacology*
  • Peptides / toxicity
  • Scorpion Venoms / genetics
  • Scorpion Venoms / metabolism
  • Scorpion Venoms / pharmacology*
  • Scorpion Venoms / toxicity
  • Scorpions / genetics
  • Scorpions / metabolism*
  • Simian Immunodeficiency Virus / drug effects*
  • Simian Immunodeficiency Virus / growth & development
  • Simian Immunodeficiency Virus / immunology
  • Transcriptome
  • Virus Replication / drug effects*

Substances

  • Anti-Retroviral Agents
  • Cytokines
  • Inflammation Mediators
  • Peptides
  • Scorpion Venoms